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Results for "

Pain behavior

" in MedChemExpress (MCE) Product Catalog:

60

Inhibitors & Agonists

1

Biochemical Assay Reagents

8

Peptides

3

Natural
Products

3

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-109061
    Lazertinib
    3 Publications Verification

    YH25448; GNS-1480

    		 Apoptosis Akt TRP Channel EGFR ERK Infection Neurological Disease Metabolic Disease Cancer
    Lazertinib (YH25448; GNS-1480) is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
    Lazertinib
  • HY-142240
    Crisugabalin

    HSK16149

    		 Calcium Channel Neurological Disease
    Crisugabalin is an orally active, selective ligand for the α2δ subunit of voltage-gated calcium channels, with a target IC50 of 3.96 nM in rats. Crisugabalin inhibits the binding of [ 3H]gabapentin to the α2δ subunit, reduces calcium influx, decreases neuronal excitability, and impairs nociceptive transmission. Crisugabalin alleviates mechanical allodynia, neuropathic pain and inflammatory pain in rats, and reduces phase II pain behaviors. Crisugabalin can be used in research related to chronic pain, neuropathic pain, diabetic neuropathy, fibromyalgia, inflammatory pain, diabetic peripheral neuropathy and postherpetic neuralgia.
    Crisugabalin
  • HY-B0168A
    Milnacipran hydrochloride
    2 Publications Verification

    		 Serotonin Transporter PERK Neurological Disease
    Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .
    Milnacipran hydrochloride
  • HY-103175
    PSB36
    1 Publications Verification

    		 Adenosine Receptor Cardiovascular Disease Neurological Disease Inflammation/Immunology
    PSB36 is a highly selective A1 adenosine receptor antagonist, with a Ki of 0.12 nM and a Kd of 0.7 nM. Systemic administration of PSB36 reduces formalin- and Carrageenan (HY-125474)-induced edema in mice and decreases pain-related behaviors, with no local paw activity. PSB36 prolongs the APD90 of rat and human atria, produces a frequency-dependent prolongation of rat atrial ERP, increases the diastolic threshold of rat atria, and shortens the duration of atrial fibrillation episodes. PSB36 can be used in research related to inflammatory pain, inflammatory hyperalgesia, edema and atrial fibrillation .
    PSB36
  • HY-W250122
    Glutamic acid sodium salt
    1 Publications Verification

    Monosodium glutamate

    		 Biochemical Assay Reagents Reactive Oxygen Species (ROS) Mitochondrial Metabolism Apoptosis HSP Bcl-2 Family Neurological Disease Metabolic Disease Inflammation/Immunology
    Glutamic acid sodium salt (Monosodium glutamate) is an orally active food flavor enhancer. Glutamic acid sodium salt causes ROS generation, mitochondrial dysfunction, and Apoptosis. Glutamic acid sodium salt upregulates CHOP, Grp78, and Bcl-2. Glutamic acid sodium salt impairs cognition, induces depressive-like behavior, induces hyperalgesia, and induces obesity and insulin resistance. Glutamic acid sodium salt can be used to study neurotoxicity (e.g., brain damage, cognitive impairment), metabolic disorders (e.g., obesity, insulin resistance), hepatotoxicity, and renal toxicity, as well as pain-related disorders .
    Glutamic acid sodium salt
  • HY-100903
    Norbinaltorphimine dihydrochloride
    5+ Cited Publications

    nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride

    		 Opioid Receptor Neurological Disease
    Norbinaltorphimine dihydrochloride (nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride) is a selective, long-acting competitive antagonist of the κ-opioid receptor. Norbinaltorphimine dihydrochloride blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. Norbinaltorphimine dihydrochloride suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. Norbinaltorphimine dihydrochloride is applicable to research related to neurological disorders such as pain .
    Norbinaltorphimine dihydrochloride
  • HY-117040
    nor-Binaltorphimine
    5+ Cited Publications

    Norbinaltorphimine; NorBNI

    		 Opioid Receptor Neurological Disease
    nor-Binaltorphimine (Norbinaltorphimine; NorBNI) is a selective, long-acting competitive antagonist of the κ-opioid receptor. nor-Binaltorphimine blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. nor-Binaltorphimine suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. nor-Binaltorphimine is applicable to research related to neurological disorders such as pain .
    nor-Binaltorphimine
  • HY-120380
    FeTMPyP

    		MOFs PARP Neurological Disease
    FeTMPyP is an orally active poly (ADP-ribose) polymerase (PARP) inhibitor. FeTMPyP inhibits cell death, nitrotyrosine formation, and depolarization of mitochondrial transmembrane potential. FeTMPyP reduces homocysteine-induced nitrosative stress and partially restores TFEB protein and mRNA levels. FeTMPyP improves functional and behavioral deficits caused by chronic constriction injury in rats. FeTMPyP alleviates acute cerebral infarction in a rat model of middle cerebral artery occlusion with mild hyperglycemia. FeTMPyP can be used in studies related to neuropathic pain, renal aging, ischemic penumbra, and hyperglycemic stroke .
    FeTMPyP
  • HY-18101A
    BD-1063 dihydrochloride
    3 Publications Verification

    		 Sigma Receptor TRP Channel Neurological Disease
    BD-1063 dihydrochloride is a selective σ-1 receptor antagonist with inhibitory activity against TRPC5 and TRPM3. BD-1063 dihydrochloride exerts anti-hyperalgesic and anti-allodynic effects by inhibiting sustained calcium influx mediated by TRPC5 and TRPM3, and reverses the effects of Carrageenan (HY-125474). BD-1063 dihydrochloride also significantly reduces excessive ethanol self-administration behavior. BD-1063 dihydrochloride is widely used in studies on the mechanisms underlying neuropathic pain, inflammatory hyperalgesia, and alcohol abuse and dependence .
    BD-1063 dihydrochloride
  • HY-P10638
    TAT-CN21

    		CaMK Cardiovascular Disease Neurological Disease
    TAT-CN21 is a potent CaMKII inhibitor with an IC50 of 77.2 nM. TAT-CN21 inhibits both calcium/calmodulin-dependent and autonomously activated CaMKII, blocks glutamate-induced translocation of CaMK IIα, and reverses the enhanced phosphorylation of CaMKII at Thr286 following excitotoxic injury. TAT-CN21 shows application potential in studies related to ischemic stroke by reducing neuronal excitotoxicity and exacerbating pre-existing long-term neuronal death prior to injury. TAT-CN21 improves definitive behaviors in rats with residual nerve injury without altering indicators such as mechanical/thermal hyperalgesia or spatial memory. TAT-CN21 can also be used in studies related to neuropathic pain .
    TAT-CN21
  • HY-109061B
    Lazertinib mesylate
    3 Publications Verification

    YH25448 mesylate; GNS-1480 mesylate

    		 TRP Channel EGFR Akt ERK Apoptosis Cancer
    Lazertinib (YH25448; GNS-1480) mesylate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
    Lazertinib mesylate
  • HY-103111
    MMPIP hydrochloride

    		mGluR Neurological Disease
    MMPIP hydrochloride is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP hydrochloride acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP hydrochloride alleviates pain and normalizes affective and cognitive behavior in neuropathic mice .
    MMPIP hydrochloride
  • HY-N2571
    Corydine

    		Reverse Transcriptase HIV Opioid Receptor Infection Neurological Disease Cancer
    Corydine is a HIV-1 reverse transcriptase inhibitor and μ-opioid receptor (MOR) agonist, with an IC50 of 356.7 μg/mL against HIV-1 reverse transcriptase, an EC50 of 0.51 μM for MOR, and a Ki of 2.82 μM for MOR. Corydine produces antinociceptive effects by inhibiting acetic acid-induced writhing behavior in a MOR-dependent manner. Corydine inhibits the proliferation of cancer cells, mitogen-stimulated lymphocytes and IL-2-dependent cells. Corydine can be used in studies related to human immunodeficiency virus infection, visceral pain, leukemia, melanoma, bladder cancer and colon adenocarcinoma .
    Corydine
  • HY-B1752
    Quinpirole
    4 Publications Verification

    LY 171555; (-)-LY 141865

    		 Dopamine Receptor Calcium Channel Bcl-2 Family iGluR Apoptosis Neurological Disease
    Quinpirole (LY 171555; (-)-LY 141865) is a D2/D3 dopamine receptor agonist and a CaV1.3 calcium channel modulator. Quinpirole normalizes dendritic spine density in dopamine-depleted striatum, upregulates the protein expression of BCL2 and GluR2, downregulates the protein expression of BAX, and delays the onset of seizures. Quinpirole enhances learning and memory, inhibits neuronal apoptosis (apoptosis), and induces anxiety-like, stereotyped, and compulsive behaviors. Quinpirole disrupts prepulse inhibition in rhesus monkeys, enhances the activity of paraventricular thalamic neurons to promote recovery from Isoflurane anesthesia, and alters the composition of the gut microbiota in rats. Quinpirole can be used in research related to dyskinesia, pain, epilepsy, and neurological disorders including anxiety disorder, obsessive-compulsive disorder, and schizophrenia .
    Quinpirole
  • HY-N5025
    Bullatine A

    		P2X Receptor Apoptosis ERK p38 MAPK c-Myc NF-κB Reactive Oxygen Species (ROS) Neurological Disease Inflammation/Immunology Cancer
    Bullatine A, a diterpenoid alkaloid, is a potent P2X7 antagonist. Bullatine A possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A inhibits ATP-induced BV-2 cell death/apoptosis and P2X receptor-mediated inflammatory responses. Bullatine A suppresses glioma cell growth by targeting SIRT6. Bullatine A specifically attenuates pain hypersensitivity in rats. Bullatine A attenuates LPS (HY-D1056)-induced systemic inflammatory response by inhibiting the ROS/JNK/NF-κB pathway in mice. Bullatine A improves despair behavior in Chronic chronic social defeat stress (CSDS) mice. Bullatine A can be used for the study of inflammation, glioblastoma (GBM) and depression .
    Bullatine A
  • HY-108519
    AS1892802

    		ROCK Neurological Disease
    AS1892802 is a potent, orally active, and highly selective inhibitor of ROCK. The onset of antinociceptive effect of AS1892802 is as fast as those of Tramadol and Diclofenac. AS1892802 did not induce gastric irritation or abnormal behavior. AS1892802 is an attractive analgesic profile for the research of severe osteoarthritis pain .
    AS1892802
  • HY-114269
    (-)-(S)-B-973B

    		nAChR Neurological Disease Inflammation/Immunology
    (-)-(S)-B-973B is an allosteric activator of α7 nicotinic acetylcholine receptor (α7 nAChR). (-)-(S)-B-973B alleviates pain behaviors. (-)-(S)-B-973B can be used for the research of inflammatory pain .
    (-)-(S)-B-973B
  • HY-107503
    MMPIP

    		mGluR Neurological Disease
    MMPIP is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP alleviates pain and normalizes affective and cognitive behavior in neuropathic mice .
    MMPIP
  • HY-131879
    NS383

    		Sodium Channel Neurological Disease
    NS383 is a potent and uniquely selective inhibitor of rat ASICs containing 1a and/or 3 subunits. NS383 inhibits H(+)-activated currents recorded from rat homomeric ASIC1a, ASIC3, and heteromeric ASIC1a+3 with IC50 values ranging from 0.61 to 2.2 μM. NS383 is well tolerated and capable of reversing pathological painlike behaviors, presumably via peripheral actions, but possibly also via actions within central pain circuits .
    NS383
  • HY-W021450A
    DL-Fluorocitric acid barium

    		Biochemical Assay Reagents Neurological Disease
    DL-Fluorocitric acid barium is a glial cell metabolic inhibitor. DL-Fluorocitric acid barium inhibits mechanical hyperalgesia induced by subcutaneous injection of complete Freund's adjuvant in rats. DL-Fluorocitric acid barium inhibits nociceptive behaviors induced by Histamine (HY-B1204) in mice and blocks the phosphorylation of the NMDA receptor NR1 subunit in the lumbar spinal cord of mice. DL-Fluorocitric acid (barium) can be used in the research of mechanical hyperalgesia and nociceptive pain .
    DL-Fluorocitric acid barium
  • HY-108960
    PPADS

    		P2X Receptor Interleukin Related Neurological Disease
    PPADS is a P2X receptor (P2X Receptor) antagonist and a reversible competitive antagonist of NAADP receptors, with IC50 values of 68 nM (P2X1) and 214 nM (P2X3), respectively. PPADS alleviates pain-related behaviors in the central and peripheral nervous systems of mice after peripheral neuropathy, inhibits the overproduction of IL-1β, IL-6, iNOS and nNOS, and suppresses the hydrolytic activity of extracellular ATPase. PPADS blocks ATP-mediated inward currents on recombinant rat P2X1 and P2X3 receptors, and inhibits purinergic nerve stimulation-induced contraction of rabbit bladder detrusor muscle. PPADS is applicable to research related to neuropathic pain .
    PPADS
  • HY-B0168
    Milnacipran
    2 Publications Verification

    		 Serotonin Transporter PERK Neurological Disease
    Milnacipran is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran inhibits pERK1/2 activation. Milnacipran has antidepressant, anxiolytic and analgesic properties. Milnacipran inhibits biting behavior in mice. Milnacipran can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .
    Milnacipran
  • HY-W010989
    Gly-His-Lys acetate

    		Biochemical Assay Reagents Bacterial Infection Neurological Disease Inflammation/Immunology Cancer
    Gly-His-Lys acetate is a natural, circulating regulatory and antimicrobial tripeptide derived from extracellular matrix proteins. Gly-His-Lys acetate binds Cu 2+ to support copper enzyme activation, antioxidant processes, cellular bioenergetics, and the synthesis of elastin, collagen and catecholamines. Gly-His-Lys acetate regulates cell growth, differentiation and tissue repair, and exerts regenerative, anxiolytic, anti-inflammatory, analgesic and immunosuppressive activities. Gly-His-Lys acetate induces liver degenerative changes. Gly-His-Lys acetate can be used for the research of infections, anxiety, pain-related behaviors and immune-associated liver diseases .
    Gly-His-Lys acetate
  • HY-15691
    PF-04455242

    		Opioid Receptor mTOR Neurological Disease Metabolic Disease
    PF-04455242 is an orally bioavailable, blood-brain barrier-permeable κ-opioid receptor (KOR) inhibitor. PF-04455242 blocks in vivo effects induced by KOR and MOR agonists, and elicits KOR-independent outward currents in ventral tegmental area neurons. PF-04455242 promotes energy expenditure and activates the hypothalamic mTOR pathway. PF-04455242 attenuates stress-induced behavioral effects and produces antidepressant-like effects. PF-04455242 can be used in studies related to pain, depression, addictive disorders, and obesity induced by estrogen withdrawal .
    PF-04455242
  • HY-N8852
    6-Methoxyflavanone

    6-MeOF

    		 GABA Receptor Taste Receptor Neurological Disease Metabolic Disease
    6-Methoxyflavanone (6-MeOF) is a flavonoid compound that can cross the blood-brain barrier. 6-Methoxyflavanone is a positive allosteric modulator of GABAA receptors. 6-Methoxyflavanone exhibits positive allosteric regulatory effects on human recombinant α1β2γ2L and α2β2γ2L GABAA receptors, and is relatively inactive on the α1β2 GABAA receptor. 6-Methoxyflavanone showes inhibitory behavior towards the activation of bitter receptor hTAS2R39 and hTAS2R14, demonstrating a reversible and non-overcome antagonistic effect. 6-Methoxyflavanone has the effects of anti-anxiety, analgesia and relief of neuropathic pain .
    6-Methoxyflavanone
  • HY-P1216
    HS014

    		Melanocortin Receptor Neurological Disease
    HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats .
    HS014
  • HY-143880
    MRGPRX1 agonist 4

    		Mas-related G-protein-coupled Receptor (MRGPR) Neurological Disease
    MRGPRX1 agonist 4 (compound 1t) is a potent and orally active Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC50 value of 0.1 μM. MRGPRX1 agonist 4 has good metabolic stability and oral bioavailability. MRGPRX1 agonist 4 can reduce behavioral heat hypersensitivity in a neuropathic pain model humanized MRGPRX1 mice. MRGPRX1 agonist 4 can be used for researching neuropathic pain .
    MRGPRX1 agonist 4
  • HY-P1216A
    HS014 TFA
    1 Publications Verification

    		 Melanocortin Receptor Neurological Disease
    HS014 TFA is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors respectively. HS014 TFA increases food intake in free-feeding rats .
    HS014 TFA
  • HY-159171
    sEH/HDAC6-IN-2

    		Epoxide Hydrolase HDAC Neurological Disease Inflammation/Immunology
    sEH/HDAC6-IN-2 is a potent dual soluble epoxide hydrolase (sEH) and HDAC6 inhibitor with IC50s of 0.9 nM, 46.8 nM, and 8 nM for human sEH, mouse sEH, and HDAC6, respectively. sEH/HDAC6-IN-2 can be used for the study of inflammatory pain .
    sEH/HDAC6-IN-2
  • HY-14343
    KLYP961

    		NO Synthase Neurological Disease
    KLYP961 is a selective and orally active dual inhibitor of inducible and neuronal NO synthase (IC50 = 50-400 nM). KLYP961 can inhibit endotoxin-evoked plasma nitrates increases and attenuate pain behaviors in a mouse formalin model. KLYP961 can attenuate carrageenin-induced edema and inflammatory hyperalgesia and writhing response elicited by Phenylbenzoquinone (HY-W275039). KLYP961 can be used for the research of neurological disease .
    KLYP961
  • HY-B0168S
    Milnacipran-d10 hydrochloride

    		Isotope-Labeled Compounds Serotonin Transporter PERK Neurological Disease
    Milnacipran-d10 (hydrochloride) is the deuterium labeled Milnacipran hydrochloride (HY-B0168A). Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .
    Milnacipran-d10 hydrochloride
  • HY-P1426
    AmmTX3

    		Potassium Channel Neurological Disease
    AmmTX3 is a peptide toxin identified from the venom of the scorpion Androctonus mauretanicus. AmmTX3 is a highly specific blocker of Kv4 channels, which selectively and almost completely blocks transient A-type K + currents with a Ki of 131 nM. AmmTX3 induces epileptiform behaviors and causes death in mice receiving intracerebroventricular injection. AmmTX3 increases the excitability of dentate gyrus granule cells, reduces GABAergic inhibition, enhances and stabilizes the EPSP-spike component of long-term potentiation, and impairs reference memory. AmmTX3 can be used in research related to pain, epilepsy, and autism spectrum disorder .
    AmmTX3
  • HY-P11642A
    Sialorphin TFA

    		Enteropeptidase Aminopeptidase Opioid Receptor ERK mTOR Androgen Receptor Inflammation/Immunology
    Sialorphin TFA is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin TFA blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin TFA regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin TFA exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin TFA also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin TFA is also a copper (II) ion-binding ligand. Sialorphin TFA has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease .
    Sialorphin TFA
  • HY-171807
    TC-2559 free base

    		nAChR STAT Neurological Disease Inflammation/Immunology
    TC-2559 free base is a α4β2 nicotinic acetylcholine receptor (nAChR) agonists with an EC50 of 0.18 μM. TC-2559 free base shows much weaker potencies on the group of b4-containing nAChR subtypes, α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. TC-2559 free base can increase the discharge of dopamine cells in the ventral tegmental area (VTA) of rats in vitro, enhancing the excitability and aggressive behavior of VTA dopamine neurons. TC-2559 free base inhibits STAT3 to exert anti-inflammatory properties and relieves mice mechanical allodynia and improve rats cognitive deficits. TC-2559 free base can be used for the study of nerve pain .
    TC-2559 free base
  • HY-111256
    A-850002

    		mGluR Neurological Disease
    A-850002 is a metabotropic glutamate receptor (mGluR) antagonist (IC50=27 nM) that significantly attenuates spontaneous pain behavior after skin incision in rats. A-850002 can be used for analgesia research .
    A-850002
  • HY-124406
    A-794282

    		mGluR Neurological Disease
    A-794282 is a compound with analgesic activity and is a selective mGlu1 receptor antagonist that significantly reduces pain behaviors in a postoperative pain model, but motor side effects may occur at higher doses.
    A-794282
  • HY-108425A
    AMG8380

    		Sodium Channel Neurological Disease
    AMG8380, an orally active and less active enantiomer of AMG8379, can serves as a negative control. AMG8380 inhibits human and mouse voltage-gated sodium channel NaV1.7 with IC50s of 0.907 and 0.387 μM, respectively. AMG8380 blocks Tetrodotoxin (TTX)-sensitive native channels with an IC50 of 2560 nM .
    AMG8380
  • HY-162347
    Nav1.7-IN-13

    		Sodium Channel Neurological Disease
    Nav1.7-IN-13 (compound 3g) is a sodium channel inhibitor that significantly inhibits Veratridine (HY-N6691)-induced neuronal activity. Nav1.7-IN-13 inhibits total Na+ current in DRG neurons in a concentration-dependent manner; slows down the activation of Navs. Nav1.7-IN-13 significantly alleviated mechanical pain behavior in a rat model of nerve injury (SNI) and had analgesic activity .
    Nav1.7-IN-13
  • HY-15691A
    PF-4455242 hydrochloride

    		Opioid Receptor mTOR Neurological Disease Metabolic Disease
    PF-4455242 hydrochloride is an orally bioavailable, blood-brain barrier-permeable κ-opioid receptor (KOR) inhibitor. PF-4455242 hydrochloride blocks in vivo effects induced by KOR and MOR agonists, and elicits KOR-independent outward currents in ventral tegmental area neurons. PF-4455242 hydrochloride promotes energy expenditure and activates the hypothalamic mTOR pathway. PF-4455242 hydrochloride attenuates stress-induced behavioral effects and produces antidepressant-like effects. PF-4455242 hydrochloride can be used in studies related to pain, depression, addictive disorders, and obesity induced by estrogen withdrawal .
    PF-4455242 hydrochloride
  • HY-B0168AS
    Milnacipran-d5 hydrochloride

    		Isotope-Labeled Compounds Serotonin Transporter PERK Neurological Disease
    Milnacipran-d5 hydrochloride is deuterium labeled Milnacipran hydrochloride (HY-B0168A). Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .
    Milnacipran-d5 hydrochloride
  • HY-P1426A
    AmmTX3 TFA

    		Potassium Channel Neurological Disease
    AmmTX3 TFA is a peptide toxin identified from the venom of the scorpion Androctonus mauretanicus. AmmTX3 TFA is a highly specific blocker of Kv4 channels, which selectively and almost completely blocks transient A-type K + currents with a Ki of 131 nM. AmmTX3 TFA induces epileptiform behaviors and causes death in mice receiving intracerebroventricular injection. AmmTX3 TFA increases the excitability of dentate gyrus granule cells, reduces GABAergic inhibition, enhances and stabilizes the EPSP-spike component of long-term potentiation, and impairs reference memory. AmmTX3 TFA can be used in research related to pain, epilepsy, and autism spectrum disorder .
    AmmTX3 TFA
  • HY-B0168AR
    Milnacipran hydrochloride (Standard)

    		Reference Standards Serotonin Transporter PERK Neurological Disease
    Milnacipran (hydrochloride) (Standard) is the analytical standard of Milnacipran hydrochloride (HY-B0168A). This product is intended for research and analytical applications. Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .
    Milnacipran hydrochloride (Standard)
  • HY-103111R
    MMPIP hydrochloride (Standard)

    		Reference Standards mGluR Neurological Disease
    MMPIP hydrochloride (Standard) is the analytical standard of MMPIP hydrochloride (HY-103111). This product is intended for research and analytical applications. MMPIP hydrochloride is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP hydrochloride acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP hydrochloride alleviates pain and normalizes affective and cognitive behavior in neuropathic mice .
    MMPIP hydrochloride (Standard)
  • HY-108519R
    AS1892802 (Standard)

    		Reference Standards ROCK Neurological Disease
    AS1892802 (Standard) is the analytical standard of AS1892802 (HY-108519). This product is intended for research and analytical applications. AS1892802 is a potent, orally active, and highly selective inhibitor of ROCK. The onset of antinociceptive effect of AS1892802 is as fast as those of Tramadol and Diclofenac. AS1892802 did not induce gastric irritation or abnormal behavior. AS1892802 is an attractive analgesic profile for the research of severe osteoarthritis pain .
    AS1892802 (Standard)
  • HY-183566
    MK-5661

    		Sodium Channel Neurological Disease
    MK-5661 is an orally potent NaV1.8 voltage-gated sodium channel inhibitor with an EC50 of 4.3 nM. MK-5661 selectively inhibits peripheral nociceptive signaling mediators. MK-5661 reduces capsaicin-induced spontaneous nociceptive behaviors in humanized rats and attenuates capsaicin-induced skin flushing responses in rhesus monkeys. MK-5661 is applicable for pain-related research .
    MK-5661
  • HY-122692
    TRPV4/TRPA1-IN-1

    		TRP Channel Neurological Disease Inflammation/Immunology
    TRPV4/TRPA1-IN-1 is a TRPV4/TRPA1 inhibitor that suppresses TRPV4/TRPA1-mediated calcium influx. TRPV4/TRPA1-IN-1 alleviates pain behaviors in a mouse trigeminal stimulation pain model and inhibits inflammation and pain-related behaviors in a mouse acute pancreatitis model. TRPV4/TRPA1-IN-1 can be used in research on acute pancreatitis .
    TRPV4/TRPA1-IN-1
  • HY-182710
    DA-0218

    		Sodium Channel Neurological Disease
    DA-0218 is a Nav1.7 inhibitor. DA-0218 exerts state-dependent inhibitory effects. DA-0218 alleviates formalin-induced inflammatory pain behavior and Paclitaxel-induced mechanical hyperalgesia in mice. DA-0218 inhibits Histamine-induced acute pruritus and lymphoma-induced chronic pruritus in mice. DA-0218 can be used in research related to inflammatory pain, neuropathic pain, acute pruritus and chronic pruritus .
    DA-0218
  • HY-183652
    5-HT2C-agonist-14

    		5-HT Receptor Sodium Channel Neurological Disease
    5-HT2C-agonist-14 is a 5-HT2C receptor agonist with an EC50 of 2.9 μM against human receptors. It also acts as a voltage-gated sodium channel inhibitor with blood-brain barrier permeable. 5-HT2C-agonist-14 elevates seizure threshold, suppresses seizure progression and alleviates pain-related behaviors. It can be used in the research of epilepsy and pain-related diseases .
    5-HT2C-agonist-14
  • HY-180802
    BCFTP

    		Mas-related G-protein-coupled Receptor (MRGPR) Neurological Disease
    BCFTP is a potent, orally active and selective human Mas-related G protein-coupled receptor X1 (MrgprX1)-positive allosteric modulator. BCFTP selectively potentiates MrgprX1 signaling in HEK293 cells. BCFTP alleviates specific neuropathic pain-related behaviors in a humanized MrgprX1 mouse model of chronic constrictive injury (CCI) in a MrgprX1-dependent manner. BCFTP synergistically enhances psychoactive substances analgesia in CCI MrgprX1 mice. BCFTP can be used for neuropathic pain research .
    BCFTP
  • HY-181482
    A1480LS

    		DAGL Neurological Disease
    A1480LS is a peripherally restricted, orally active covalent and irreversible inhibitor of DAGLα and DAGLβ, with IC50 values of 6 nM and 4 nM against human targets, respectively, and IC50 values ≤15 nM across mouse, rat, dog, monkey and human systems. A1480LS reduces the levels of 2-arachidonoylglycerol, arachidonic acid, and cyclooxygenase- and lipoxygenase-derived eicosanoids. A1480LS inhibits injury-induced production of 2-arachidonoylglycerol and arachidonic acid in the peripheral sciatic nerve, and suppresses the responses of high-threshold and wide-dynamic-range-like dorsal horn neurons to mechanical stimulation. A1480LS alleviates pain behaviors in rat models of inflammatory pain, neuropathic pain and chemotherapy-induced peripheral neuropathy .
    A1480LS

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